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Cited by 276Protein Degradation and InhibitorsChromatin Remodeling and CancerCancer-related Molecular Pathways

Targeting Transcription Factors in Cancer

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Bhagwat, Anand S., Vakoc, Christopher R.·2015·Trends in Cancer
DOI 10.1016/j.trecan.2015.07.001PMC PMC4669894
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Abstract

Transcription factors (TFs) are commonly deregulated in the pathogenesis of human cancer and are a major class of cancer cell dependencies. Consequently, targeting of TFs can be highly effective in treating particular malignancies, as highlighted by the clinical efficacy of agents that target nuclear hormone receptors. In this review we discuss recent advances in our understanding of TFs as drug targets in oncology, with an emphasis on the emerging chemical approaches to modulate TF function. The remarkable diversity and potency of TFs as drivers of cell transformation justifies a continued pursuit of TFs as therapeutic targets for drug discovery.

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  • Recent advancements in drug discovery, such as novel chemical libraries and protein engineering techniques, are paving the way for overcoming obstacles to targeting transcription factors.

    “However, recent advancements in drug discovery, such as the development of novel chemical libraries and protein engineering techniques, are paving the way for overcoming these obstacles [15, 17, 18].”

    From Targeting Microglial Transcriptional Reprogramming as a Therapy Strategy for Alzheimer's Disease (2026) · cites this paper as [17]

    The Introduction and Concluding Remarks describe emerging chemical strategies and high-throughput chemical screens as ways to target transcription factors. They do not identify novel chemical libraries or protein engineering techniques as the advances overcoming these obstacles; no page numbers are supplied in our copy. (LLM, conf=0.87)

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Cited by

Sorted by citations

Authors
Bhagwat, A. S., & Vakoc, C. R.
Affiliations
Cold Spring Harbor Laboratory (US)
Corresponding author
Vakoc, Christopher R.
ORCID
Venue
Trends in Cancer
Publisher
Elsevier BV
Published
2015-09
Volume
1
Issue
1
Pages
53-65
ISSN
  • 2405-8025 (ISSN-L)
  • 2405-8033
DOI
10.1016/j.trecan.2015.07.001
PMC
PMC4669894
OpenAlex
W1851611944
Cited by
276
References
13
Citations by year
2026: 8 · 2025: 21 · 2024: 25 · 2023: 22 · 2022: 32 · 2021: 32 · 2020: 29 · 2019: 23 · 2018: 39 · 2017: 33 · 2016: 11
FWCI
2.68
Type
journal article
Language
en
Open access
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations
  • Trends in cancer (publishedVersion)
  • PubMed (publishedVersion)
  • PubMed Central (acceptedVersion)
  • Cold Spring Harbor Laboratory Institutional Repository (Cold Spring Harbor Laboratory) (submittedVersion)
Funders
  • Wellcome Trust
  • National Institutes of Health (5p30ca045508-35)
  • National Cancer Institute (F30CA186632, P30-CA045508, R01CA174793)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chromatin Remodeling and Cancer
  • Health Sciences › Medicine › Oncology › Cancer-related Molecular Pathways
Keywords
transcription factors, cancer drug targets, nuclear receptors, anticancer drug discovery

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